塞克硝唑1/2水合物的研究

Study of secnidazole hemihydrate

目的 对合成的塞克硝唑进行结晶水的分析和稳定性研究。方法 以2-甲基5-硝基咪唑为原料,与1,2-环氧丙炕在85％的甲酸中反应制得塞克硝唑1/2水合物;通过卡费休水分测定法、干燥失重法、元素分析、热重分析及差热分析等方法确证产物中结晶水的含量;用药典方法进行了稳定性研究。结果 合成得到的产品为塞克硝唑1/2水合物,稳定性比无水物好,熔点与无水物有差异。结论 首次明确了1/2水合物为塞克硝唑的稳定存在形式,并明确了1/2结晶水合物和无水物的熔点差异。

OBJECTIVE To study the stability and crystal water of synthesizing secnidazole. METHODS The ti-the compound. (C7H11 N.3O3·1/2 H2O) was synthesized by the reaction of 2-methyl-5-nitroimidazole with 1 , 2-epoxy prapane in 85% formatic acid. Its half mole crystal water was determined by melting point analysis, Karl Fischer ti-tration, weight loss on drying, elemental analysis. TGA. and DSC. Its stability was studied using Chinese Pharmacopoeia. RESULTS The synthesized product was secnidazole hemihydratc, whose stability was better than its an hydrate and melting point was different. CONCLUSIONS We hevc first defined hemihydrate is the stable form of sec-nidazole, and proved the difference of melting point between secnidazole hemihydrate and its anhydratc.